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3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-02-27 , DOI: 10.1016/j.bmcl.2018.02.047 Alexander Q Cusumano 1 , Joshua G Pierce 2
中文翻译：
3-Hydroxy-1,5-dihydro- 2H -pyrrol-2-ones作为新型的耐甲氧西林金黄色葡萄球菌抗菌支架
更新日期：2018-02-27
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-02-27 , DOI: 10.1016/j.bmcl.2018.02.047 Alexander Q Cusumano 1 , Joshua G Pierce 2
Affiliation
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Herein, we report the synthesis and evaluation of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones as antibacterial agents against methicillin-resistant S. aureus (MRSA) and methicillin-resistant S. epidermidis (MRSE). Lead compound 38 showed minimum inhibitory concentrations (MICs) of 8 and 4 μg/mL against MRSA and MRSE, respectively. Furthermore, compound 38 displayed a MIC of 8–16 μg/mL against linezolid-resistant MRSA. These molecules, previously underexplored as antibacterial agents, serve as a new scaffold for antimicrobial development.
中文翻译：
3-Hydroxy-1,5-dihydro- 2H -pyrrol-2-ones作为新型的耐甲氧西林金黄色葡萄球菌抗菌支架
在此，我们报告了3-羟基-1,5-二氢-2H-吡咯-2-酮作为抗甲氧西林耐药金黄色葡萄球菌（MRSA）和耐甲氧西林表皮葡萄球菌（MRSE）的抗菌剂的合成和评估。铅化合物38对MRSA和MRSE的最小抑菌浓度（MIC）分别为8和4μg/ mL。此外，化合物38对耐利奈唑胺的MRSA的MIC为8-16μg/ mL。这些以前未被开发为抗菌剂的分子，可作为抗菌素开发的新支架。
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